LV11622A - 4-Azaandrostane derivatives are inhibitors of 5 alpha-reductase isoenzyme 1 - Google Patents

4-Azaandrostane derivatives are inhibitors of 5 alpha-reductase isoenzyme 1

Info

Publication number
LV11622A
LV11622A LV960125A LV960125A LV11622A LV 11622 A LV11622 A LV 11622A LV 960125 A LV960125 A LV 960125A LV 960125 A LV960125 A LV 960125A LV 11622 A LV11622 A LV 11622A
Authority
LV
Latvia
Prior art keywords
inhibitors
reductase
alpha
5alpha
reductase isoenzyme
Prior art date
Application number
LV960125A
Other languages
Latvian (lv)
Other versions
LV11622B (en
Inventor
Philippe L Durette
William K Hagmann
Lanza Thomas J Jr
Soumya P Sahoo
Gary H Rasmusson
Richard L Tolman
Derek Von Langen
Original Assignee
Merck & Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of LV11622A publication Critical patent/LV11622A/en
Publication of LV11622B publication Critical patent/LV11622B/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07J—STEROIDS
    • C07J73/00—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms
    • C07J73/001—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom
    • C07J73/005—Steroids in which the cyclopenta[a]hydrophenanthrene skeleton has been modified by substitution of one or two carbon atoms by hetero atoms by one hetero atom by nitrogen as hetero atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/14—Drugs for dermatological disorders for baldness or alopecia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P5/00—Drugs for disorders of the endocrine system
    • A61P5/24—Drugs for disorders of the endocrine system of the sex hormones
    • A61P5/28—Antiandrogens

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Endocrinology (AREA)
  • Diabetes (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Medicines Containing Plant Substances (AREA)

Abstract

Compounds of the Formula Iare inhibitors of the 5alpha-reductase 1 isozyme, and are useful alone, or in combination with a 5alpha-reductase 2 inhibitor, for the treatment of androgenic sensitive disorders such as acne vulgaris, seborrhea, female hirsutism, male pattern baldness, and benign prostatic hyperplasia.
LVP-96-125A 1993-10-21 1996-04-24 16-substituted-4-aza-androstane 5-alpha-reductase 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors isozyme 1 inhibitors LV11622B (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US14115393A 1993-10-21 1993-10-21
PCT/US1994/012071 WO1995011254A1 (en) 1993-10-21 1994-10-21 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Publications (2)

Publication Number Publication Date
LV11622A true LV11622A (en) 1996-12-20
LV11622B LV11622B (en) 1997-06-20

Family

ID=22494410

Family Applications (2)

Application Number Title Priority Date Filing Date
LVP-96-125A LV11622B (en) 1993-10-21 1996-04-24 16-substituted-4-aza-androstane 5-alpha-reductase 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors isozyme 1 inhibitors
LVP-99-70A LV12316B (en) 1993-10-21 1999-04-26 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Family Applications After (1)

Application Number Title Priority Date Filing Date
LVP-99-70A LV12316B (en) 1993-10-21 1999-04-26 16-substituted-4-aza-androstane 5-alpha-reductase isozyme 1 inhibitors

Country Status (29)

Country Link
US (4) US5739137A (en)
EP (1) EP0724592B1 (en)
JP (1) JP2862376B2 (en)
KR (1) KR100363994B1 (en)
CN (1) CN1058499C (en)
AT (1) ATE175420T1 (en)
BG (1) BG61978B1 (en)
BR (2) BR9407866A (en)
CA (1) CA2173863C (en)
CY (1) CY2136B1 (en)
CZ (1) CZ292614B6 (en)
DE (1) DE69415824T2 (en)
DK (1) DK0724592T3 (en)
ES (1) ES2125495T3 (en)
FI (1) FI961697A0 (en)
HK (1) HK1009047A1 (en)
HU (1) HUT74613A (en)
IL (1) IL111357A (en)
LV (2) LV11622B (en)
NO (1) NO308037B1 (en)
NZ (1) NZ275293A (en)
PL (1) PL179611B1 (en)
RO (1) RO116197B1 (en)
RU (1) RU2142956C1 (en)
SK (1) SK281645B6 (en)
TW (1) TW413682B (en)
UA (1) UA44257C2 (en)
WO (1) WO1995011254A1 (en)
ZA (1) ZA948285B (en)

Families Citing this family (27)

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US5547957A (en) 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
UA44257C2 (en) 1993-10-21 2002-02-15 Мерк Енд Ко, Інк 16-SUBSTITUTED DERIVATIVES OF 4-AZAANDROSTANE AS INSERBATORS OF THE ISOFERMENT 5- <font face = "Symbol"> a </font> -REDUCTASE, METHOD OF INHIBITION OF 5- <font face = "Symbol" isoenzymes, the method TREATMENT METHOD AND TERMINATION reversal of androgenic alopecia, and promote hair growth in mammals, biosynthetic CONVERSION METHOD inhibition of testosterone to dihydrotestosterone in mammals, pharmaceutical compositions
US5470976A (en) * 1994-09-07 1995-11-28 Merck & Co., Inc. Process for the stereoselective reduction of steroid enelactams
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents
JPH10508586A (en) * 1994-10-21 1998-08-25 メルク エンド カンパニー インコーポレーテッド Combination type acne treatment method
US5886005A (en) * 1995-01-17 1999-03-23 Merck & Co., Inc. 4-Aza-19-norandrostane derivatives
CA2233084A1 (en) * 1995-10-19 1997-04-24 Merck & Co., Inc. 16-substituted-6-aza-steroid 5-.alpha.-reductase inhibitors
US5872126A (en) * 1996-09-06 1999-02-16 Merck & Co., Inc. Methods and compositions for treating preterm labor
US5945412A (en) * 1996-12-09 1999-08-31 Merck & Co., Inc. Methods and compositions for preventing and treating bone loss
WO1998041509A1 (en) * 1997-03-17 1998-09-24 Merck & Co., Inc. Methods and compositions for treating polycystic ovary syndrome
US5935968A (en) * 1997-03-17 1999-08-10 Merck & Co., Inc. Methods for treating polycystic ovary syndrome
CA2308070A1 (en) * 1997-10-28 1999-05-06 Merck & Co., Inc. Prevention of precipitated acute urinary retention
US6187925B1 (en) * 1997-12-23 2001-02-13 Merck & Co., Inc. Intermediates and process for the synthesis of azasteroids
AR016257A1 (en) * 1998-05-14 2001-06-20 Merck & Co Inc PROCESS FOR STERESOSELECTIVA SYNTHESIS OF ARILOXI-4-AZA-5ALFA-ANDROSTAN-3-ONAS, 16 ALFA AND 16 BETA-SUBSTITUTED AND INSUSTITUTED, AND INTERMEDIARIES SUPPLIED IN THIS PROCESS.
WO1999058550A1 (en) * 1998-05-14 1999-11-18 Merck & Co., Inc. 7beta-methyl-16beta-((4-methylsulfonyl)-phenoxy)-4-aza-5alpha-androst-1-en-3-one as a 5-alpha-reductase isozyme 1 inhibitor
US6902721B1 (en) 1998-07-10 2005-06-07 Osteoscreen, Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6838436B1 (en) 1998-07-10 2005-01-04 Osteoscreen Inc. Inhibitors of proteasomal activity for stimulating bone growth
US6462019B1 (en) 1998-07-10 2002-10-08 Osteoscreen, Inc. Inhibitors of proteasomal activity and production for stimulating bone growth
US6048869A (en) * 1998-07-29 2000-04-11 Merck & Co., Inc. Tricyclic compounds
US6268377B1 (en) 1998-09-28 2001-07-31 Merck & Co., Inc. Method for treating androgen-related conditions
US20020198215A1 (en) * 2000-10-23 2002-12-26 Lino Tavares Terazosin transdermal device and methods
EP1734963A4 (en) * 2004-04-02 2008-06-18 Merck & Co Inc Method of treating men with metabolic and anthropometric disorders
EP1865955A4 (en) * 2005-03-25 2009-04-15 Merck & Co Inc Method of treating men with testosterone supplement and 5alpha-reductase inhibitor
US20060241696A1 (en) * 2005-04-26 2006-10-26 Stjepan Krco Method of limiting hair loss and promoting hair growth
FR2910002B1 (en) * 2006-12-13 2009-01-30 Sanofi Aventis Sa NOVEL METHOD FOR THE DIASTEREOSELECTIVE OBTAINING OF A PRIMARY CHIRAL AMINE ON A STEROID
GB201102913D0 (en) 2011-02-18 2011-04-06 Univ Birmingham Novel therapeutic
TWI522102B (en) 2013-04-30 2016-02-21 長庚醫療財團法人 Use of composition for manufacturing drugs for treating or prophylactically treating acne

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US5120742A (en) * 1984-02-27 1992-06-09 Merck & Co., Inc. 17 β-acyl-4-aza-5 α-androst-1-ene-3-ones as 5 α-reductase inhibitors
IL74365A (en) * 1984-02-27 1990-07-26 Merck & Co Inc 17beta-(n-t.-butylcarbamoyl)-4-aza-5alpha-androst-1-en-3-one and pharmaceutical compositions containing it
US5571817A (en) * 1984-02-27 1996-11-05 Merck & Co., Inc. Methods of treating androgenic alopecia with finasteride [17β-N-mono-substituted-carbamoyl-4-aza-5-α-androst-1-en-ones]
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US5151429A (en) * 1984-02-27 1992-09-29 Merck & Co., Inc. 17β-acyl-4-aza-5α-androst-1-ene-3-ones as 5α reductase inhibitors
US4760071A (en) * 1984-02-27 1988-07-26 Merck & Co., Inc. 17β-N-monosubstituted carbamoyl-4-aza-5α-androst-1-en-3-ones which are active as testosterone 5α-reductase inhibitors
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US5359071A (en) * 1993-03-12 1994-10-25 Merck & Co., Inc. 15-substituted 4-azasteroids
TW369521B (en) * 1993-09-17 1999-09-11 Smithkline Beecham Corp Androstenone derivative
US5547957A (en) * 1993-10-15 1996-08-20 Merck & Co., Inc. Method of treating androgenic alopecia with 5-α reductase inhibitors
UA44257C2 (en) * 1993-10-21 2002-02-15 Мерк Енд Ко, Інк 16-SUBSTITUTED DERIVATIVES OF 4-AZAANDROSTANE AS INSERBATORS OF THE ISOFERMENT 5- <font face = "Symbol"> a </font> -REDUCTASE, METHOD OF INHIBITION OF 5- <font face = "Symbol" isoenzymes, the method TREATMENT METHOD AND TERMINATION reversal of androgenic alopecia, and promote hair growth in mammals, biosynthetic CONVERSION METHOD inhibition of testosterone to dihydrotestosterone in mammals, pharmaceutical compositions
US5525608A (en) * 1994-04-20 1996-06-11 Merck & Co., Inc. 17b-aryl-4-aza-steroid derivatives useful as 5-alpha-reductase inhibitors
US5512555A (en) * 1994-07-21 1996-04-30 Merck & Co., Inc. Method of treating sweat-related conditions using finasteride, epristeride and a cholestan-3-one
US5543417A (en) * 1994-10-21 1996-08-06 Merck & Co., Inc. Combination method of treating acne using 4-AZA-5α-cholestan-ones and 4-AZA-5α-androstan-ones as selective 5α-reductase inhibitors with anti-bacterial, keratolytic, or anti-inflammatory agents

Also Published As

Publication number Publication date
NO308037B1 (en) 2000-07-10
RU2142956C1 (en) 1999-12-20
DE69415824T2 (en) 1999-08-05
CZ292614B6 (en) 2003-11-12
EP0724592B1 (en) 1999-01-07
US5739137A (en) 1998-04-14
JP2862376B2 (en) 1999-03-03
HK1009047A1 (en) 1999-05-21
CA2173863C (en) 2003-05-13
NO961575L (en) 1996-04-19
US5910497A (en) 1999-06-08
NO961575D0 (en) 1996-04-19
BR1100217A (en) 1999-11-09
FI961697A (en) 1996-04-18
SK49696A3 (en) 1996-10-02
PL314039A1 (en) 1996-08-05
PL179611B1 (en) 2000-10-31
ZA948285B (en) 1995-06-19
SK281645B6 (en) 2001-06-11
CZ122896A3 (en) 1997-01-15
CN1136318A (en) 1996-11-20
BR9407866A (en) 1996-10-29
AU680063B2 (en) 1997-07-17
DE69415824D1 (en) 1999-02-18
CY2136B1 (en) 2002-06-21
AU8086194A (en) 1995-05-08
LV11622B (en) 1997-06-20
HU9601037D0 (en) 1996-06-28
KR100363994B1 (en) 2003-04-10
TW413682B (en) 2000-12-01
US5719158A (en) 1998-02-17
JPH09511213A (en) 1997-11-11
ES2125495T3 (en) 1999-03-01
NZ275293A (en) 1998-02-26
ATE175420T1 (en) 1999-01-15
WO1995011254A1 (en) 1995-04-27
KR960705839A (en) 1996-11-08
DK0724592T3 (en) 1999-08-30
IL111357A (en) 2001-01-28
LV12316B (en) 1999-11-20
UA44257C2 (en) 2002-02-15
CA2173863A1 (en) 1995-04-27
EP0724592A1 (en) 1996-08-07
BG100516A (en) 1996-11-29
HUT74613A (en) 1997-01-28
FI961697A0 (en) 1996-04-18
BG61978B1 (en) 1998-11-30
CN1058499C (en) 2000-11-15
US6204273B1 (en) 2001-03-20
LV12316A (en) 1999-07-20
RO116197B1 (en) 2000-11-30
IL111357A0 (en) 1994-12-29

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